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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共45条记录   Synthesis and in Vitro Photodynamic Activities of Pegylated Distyryl Boron Dipyrromethene Derivatives [作者：HE HUI; LO PUICHI; YEUNG SINLUI; FONG WINGPING; NG DENNIS K P,期刊：Journal of Medicinal Chemistry, 页码：3097-3102 , 文章类型： Article，,卷期：2011年54-8] A series of pegylated distyryl boron dipyrromethenes have been prepared and characterized. Their in vitro photodynamic activities in Tween 80 emulsions have also been investigated against HT29 human colorectal carcinoma ... Discovery of Indeno[1,2-c]quinoline Derivatives as Inhibitors of Osteoclastogenesis Induced by Receptor Activator of NF-kappa B Ligand (RANKL) [作者：TSENG CHIHHUA; LIN RUWEI; CHEN YEHLONG; WANG GWOJAW; HO MEILING; TZENG CHERNGCHYI,期刊：Journal of Medicinal Chemistry, 页码：3103-3107 , 文章类型： Article，,卷期：2011年54-8] Certain indeno[1,2-c]quinolines were synthesized and evaluated for antiosteoclastogenic activities. Among them, 6,9-dimethoxy-11H-indeno[1,2-c]quinolin-11-one (8a) and 9-methoxy-6-(methylthio)-11H-indeno[1,2-c]quinolin-1... Synopsis of Some Recent Tactical Application of Bioisosteres in Drug Design [作者：MEANWELL NICHOLAS A,期刊：Journal of Medicinal Chemistry, 页码：2529-2591 , 文章类型： Article，,卷期：2011年54-8] Identification, Characterization, and Implications of Species-Dependent Plasma Protein Binding for the Oral Hedgehog Pathway Inhibitor Vismodegib (GDC-0449) [作者：GIANNETTI ANTHONY M; WONG HARVEY; DIJKGRAAF GERRIT J P; DUEBER ERIN C; ORTWINE DANIEL F; BRAVO BRANDON J; GOULD STEPHEN E; PLISE EMILE G; LUM BERT L; MALHI VIKRAM; GRAHAM RICHARD A,期刊：Journal of Medicinal Chemistry, 页码：2592-2601 , 文章类型： Article，,卷期：2011年54-8] Vismodegib (GDC-0449) is is an orally available selective Hedgehog pathway inhibitor in development for cancer treatment. The drug is >= 95% protein bound in plasma at clinically relevant concentrations and has an approx... Highly Improved Metabolic Stability and Pharmacokinetics of Indium-111-DOTA-Gastrin Conjugates for Targeting of the Gastrin Receptor [作者：KCLENCPEITL PETRA; MANSI ROSALBA; TAMMA MARIALUISA; GMEINERSTOPAR TANJA; SOLLNERDOLENC MARIJA; WASER BEATRICE; BAUM RICHARD P; REUBI JEAN CLAUDE; MAECKE HELMUT R,期刊：Journal of Medicinal Chemistry, 页码：2602-2609 , 文章类型： Article，,卷期：2011年54-8] The development of metabolically stable radiolabeled gastrin analogues with suitable pharmacokinetics is a topic of recent research activity. These imaging vectors are of interest because the gastrin/CCK2 receptor is hig... Design, Synthesis, Biological Activity, and ADME Properties of Pyrazolo[3,4-d]pyrimidines Active in Hypoxic Human Leukemia Cells: A Lead Optimization Study [作者：RADI MARCO; DREASSI ELENA; BRULLO CHIARA; CRESPAN EMMANUELE; TINTORI CRISTINA; BERNARDO VINCENZO; VALOTI MASSIMO; ZAMPERINI CLAUDIO; DAIGL HENRY; MUSUMECI FRANCESCA; CARRARO FABIO; NALDINI ANTONELLA; FILIPPI IRENE; MAGA GIOVANNI; SCHENONE SILVIA; BOTTA MAURIZIO,期刊：Journal of Medicinal Chemistry, 页码：2610-2626 , 文章类型： Article，,卷期：2011年54-8] A family of dual Src/Abl inhibitors characterized by a substituted pyrazolo[3,4-d]pyrimidine scaffold was previously reported by us and proved to be active against several tumor cell lines. Among these compounds, a promi... Homodimeric Bis-Quaternary Heterocyclic Ammonium Salts as Potent Acetyl- and Butyrylcholinesterase Inhibitors: A Systematic Investigation of the Influence of Linker and Cationic Heads over Affinity and Selectivity [作者：CONEJOGARCIA ANA; PISANI LEONARDO; DEL CARMEN NUNEZ MARIA; CATTO MARCO; NICOLOTTI ORAZIO; LEONETTI FRANCESCO; CAMPOS JOAQUIN M; GALLO MIGUEL A; ESPINOSA ANTONIO; CAROTTI ANGELO,期刊：Journal of Medicinal Chemistry, 页码：2627-2645 , 文章类型： Article，,卷期：2011年54-8] A molecular library of quaternary ammonium salts (QASs), mainly composed of symmetrical bis-quaternary heterocyclic bromides exhibiting choline kinase ( ChoK) inhibitory activity, were evaluated for their ability to inhi... Exploring the Size Limit of Templates for Inhibitors of the M2 Ion Channel of Influenza A Virus [作者：DUQUE MARIA D; MA CHUNLONG; TORRES EVA; WANG JUN; NAESENS LIEVE; JUAREZJIMENEZ JORDI; CAMPS PELAYO; JAVIER LUQUE F; DEGRADO WILLIAM F; LAMB ROBERT A; PINTO LAWRENCE H; VAZQUEZ SANTIAGO,期刊：Journal of Medicinal Chemistry, 页码：2646-2657 , 文章类型： Article，,卷期：2011年54-8] Amantadine inhibits the M2 proton channel of influenza A virus) yet its clinical use has been limited by the rapid emergence of amantadine-resistant virus strains. We have synthesized and characterized a series of polycy... Long-Acting Lipidated Analogue of Human Pancreatic Polypeptide Is Slowly Released into Circulation [作者：BELLMANNSICKERT KATHRIN; ELLING CHRISTIAN E; MADSEN ANDREAS N; LITTLE PAUL B; LUNDGREN KARSTEN; GERLACH LARSOLE; BERGMANN RALF; HOLST BIRGITTE; SCHWARTZ THUE W; BECKSICKINGER ANNETTE G,期刊：Journal of Medicinal Chemistry, 页码：2658-2667 , 文章类型： Article，,卷期：2011年54-8] The main disadvantages of;peptide pharmaceuticals are their rapid degradation and excretion, their low hydrophilicity, and low shelf lifes. These bottlenecks can be circumvented by acylation with fatty acids (lipidation)... Analogues and Derivatives of Oncrasin-1, a Novel Inhibitor of the C-Terminal Domain of RNA Polymerase II and Their Antitumor Activities [作者：WU SHUHONG; WANG LI; GUO WEI; LIU XIAOYING; LIU JINSONG; WEI XIAOLI; FANG BINGLIANG,期刊：Journal of Medicinal Chemistry, 页码：2668-2679 , 文章类型： Article，,卷期：2011年54-8] To optimize the antitumor activity of oncrasin-1, a small molecule RNA polymerase II inhibitor, We evaluated 69 oncrasin-1 analogues for their cytotoxic activity against normal human epithelial cells and K-Ras mutant tum... Identification of 3H-Naphtho[1,2,3-de]quinoline-2,7-diones as Inhibitors of Apoptosis Signal-Regulating Kinase 1 (ASK1) [作者：VOLYNETS GALYNA P; CHEKANOV MAKSYM O; SYNYUGIN ANATOLIY R; GOLUB ANDRIY G; KUKHARENKO OLEKSANDR P; BDZHOLA VOLODYMYR G; YARMOLUK SERGIY M,期刊：Journal of Medicinal Chemistry, 页码：2680-2686 , 文章类型： Article，,卷期：2011年54-8] Apoptosis signal-regulating kinase 1 (ASK1) has recently emerged as an attractive therapeutic target for the treatment of cardiac and neurodegenerative disorders. The selective inhibitors of ASK1 may become important com... Synthesis and Evaluation of Radioligands for Imaging Brain Nociceptin/Orphanin FQ Peptide (NOP) Receptors with Positron Emission Tomography [作者：PIKE VICTOR W; RASH KAREN S; CHEN ZHAOGEN; PEDREGAL CONCEPCION; STATNICK MICHAEL A; KIMURA YASUYUKI; HONG JINSOO; ZOGHBI SAMI S; FUJITA MASAHIRO; TOLEDO MIGUEL A; DIAZ NURIA; GACKENHEIMER SUSAN L; TAUSCHER JOHANNES T; BARTH VANESSA N; INNIS ROBERT B,期刊：Journal of Medicinal Chemistry, 页码：2687-2700 , 文章类型： Article，,卷期：2011年54-8] Positron emission tomography (PET) coupled to an effective radioligand could provide an important tool for understanding possible links between neuropsychiatric disorders and brain NOP (nociceptin/orphanin FQ peptide) re... Developing Potent Human Uric Acid Transporter 1 (hURAT1) Inhibitors [作者：WEMPE MICHAEL F; JUTABHA PROMSUK; QUADE BETTINA; IWEN TIMOTHY J; FRICK MORIN M; ROSS IAN R; RICE PETER J; ANZAI NAOHIKO; ENDOU HITOSHI,期刊：Journal of Medicinal Chemistry, 页码：2701-2713 , 文章类型： Article，,卷期：2011年54-8] The kidneys are a vital organ in the human body. They serve several purposes including homeostatic functions such as regulating extracellular fluid volume and maintaining acid-base and electrolyte balance and are essenti... A Potent and Orally Active Antagonist (SM-406/AT-406) of Multiple Inhibitor of Apoptosis Proteins (IAPs) in Clinical Development for Cancer Treatment [作者：CAI QIAN; SUN HAIYING; PENG YUEFENG; LU JIANFENG; NIKOLOVSKACOLESKA ZANETA; MCEACHERN DONNA; LIU LIU; QIU SU; YANG CHAOYIE; MILLER REBECCA; YI HAN; ZHANG TAO; SUN DUXIN; KANG SANMAO; GUO MING; LEOPOLD LANCE; YANG DAJUN; WANG SHAOMENG,期刊：Journal of Medicinal Chemistry, 页码：2714-2726 , 文章类型： Article，,卷期：2011年54-8] We report the discovery and characterization of SM-406 (compound 2), a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). This compound binds to XIAP, cIAP1, and ... Crystal Structure of tert-Butyldimethylsilyl-spiroaminooxathioledioxide-thymine (TSAO-T) in Complex with HIV-1 Reverse Transcriptase (RT) Redefines the Elastic Limits of the Non-nucleoside Inhibitor-Binding Pocket [作者：DAS KALYAN; BAUMAN JOSEPH D; RIM ANGELA S; DHARIA CHHAYA; CLARK ARTHUR D JR; CAMARASA MARIAJOSE; BALZARINI JAN; ARNOLD EDDY,期刊：Journal of Medicinal Chemistry, 页码：2727-2737 , 文章类型： Article，,卷期：2011年54-8] tert-Butyldimethylsilyl-spiroaminooxathioledioxide (TSAO) compounds have an embedded thymidine-analogue backbone; however, TSAO compounds invoke non-nucleoside RT inhibitor (NNRTI) resistance mutations. Our crystal struc... Synthesis and Separation of the Enantiomers of the Neuropeptide S Receptor Antagonist (9R/S)-3-Oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine-7-carboxylic Acid 4-Fluoro-benzylamide (SHA 68) [作者：TRAPELLA CLAUDIO; PELA MICHELA; DEL ZOPPO UISA; CALO GIROLAMO; CAMARDA VALERIA; RUZZA CHIARA; CAVAZZINI ALBERLO; COSTA VALENTINA; BERTOLASI VALERIO; REINSCHEID RAINER K; SALVADORI SEVERO; GUERRINI REMO,期刊：Journal of Medicinal Chemistry, 页码：2738-2744 , 文章类型： Article，,卷期：2011年54-8] This study reports the synthesis, chromatographic separation, and pharmacological evaluation of the two enantiomers of the neuropeptide S receptor (NPSR) antagonist (9R/S)-3-oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyra...